The plasma–occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, α5IA, is similar in rats and primates

Rat plasma EC(50) values did not vary as a function of time indicating that alpha5IA dissociates readily for the GABA(A) receptor in vivo. These data also suggest that despite the different assays used (terminal assays of [(3)H]flumazenil in vivo binding in rats and [(123)I]iomazenil gamma-scintigraphy in anaesthetized rhesus monkeys), these techniques produced similar plasma alpha5IA EC(50) values (52 and 57 ngxmL(-1) respectively) and that the plasma-occupancy relationship for alpha5IA translates across these two species.